Nature Communications (Jan 2019)
Lattice engineering enables definition of molecular features allowing for potent small-molecule inhibition of HIV-1 entry
- Yen-Ting Lai,
- Tao Wang,
- Sijy O’Dell,
- Mark K. Louder,
- Arne Schön,
- Crystal S. F. Cheung,
- Gwo-Yu Chuang,
- Aliaksandr Druz,
- Bob Lin,
- Krisha McKee,
- Dongjun Peng,
- Yongping Yang,
- Baoshan Zhang,
- Alon Herschhorn,
- Joseph Sodroski,
- Robert T. Bailer,
- Nicole A. Doria-Rose,
- John R. Mascola,
- David R. Langley,
- Peter D. Kwong
Affiliations
- Yen-Ting Lai
- Vaccine Research Center, NIAID, National Institutes of Health
- Tao Wang
- Departments of Discovery Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development
- Sijy O’Dell
- Vaccine Research Center, NIAID, National Institutes of Health
- Mark K. Louder
- Vaccine Research Center, NIAID, National Institutes of Health
- Arne Schön
- Department of Biology, Johns Hopkins University
- Crystal S. F. Cheung
- Vaccine Research Center, NIAID, National Institutes of Health
- Gwo-Yu Chuang
- Vaccine Research Center, NIAID, National Institutes of Health
- Aliaksandr Druz
- Vaccine Research Center, NIAID, National Institutes of Health
- Bob Lin
- Vaccine Research Center, NIAID, National Institutes of Health
- Krisha McKee
- Vaccine Research Center, NIAID, National Institutes of Health
- Dongjun Peng
- Vaccine Research Center, NIAID, National Institutes of Health
- Yongping Yang
- Vaccine Research Center, NIAID, National Institutes of Health
- Baoshan Zhang
- Vaccine Research Center, NIAID, National Institutes of Health
- Alon Herschhorn
- Department of Cancer Immunology and Virology, Dana–Farber Cancer Institute, Harvard Medical School
- Joseph Sodroski
- Department of Cancer Immunology and Virology, Dana–Farber Cancer Institute, Harvard Medical School
- Robert T. Bailer
- Vaccine Research Center, NIAID, National Institutes of Health
- Nicole A. Doria-Rose
- Vaccine Research Center, NIAID, National Institutes of Health
- John R. Mascola
- Vaccine Research Center, NIAID, National Institutes of Health
- David R. Langley
- Computer Assisted Drug Design, Bristol-Myers Squibb Research and Development
- Peter D. Kwong
- Vaccine Research Center, NIAID, National Institutes of Health
- DOI
- https://doi.org/10.1038/s41467-018-07851-1
- Journal volume & issue
-
Vol. 10,
no. 1
pp. 1 – 11
Abstract
Temsavir, a compound that inhibits HIV entry by binding envelope (Env), is currently in clinical development. Here, Lai et al. identify a more than 10-fold improved compound and, using lattice engineering, obtain crystal structures that give insights into improved inhibition between small molecules and Env.
